Singlon: instructions for use, analogues and reviews, prices in Russian pharmacies. Singlon: instructions for use Storage conditions and shelf life

film-coated tablets

Owner/Registrar

GEDEON RICHTER, Plc.

International Classification of Diseases (ICD-10)

J45 Asthma

Pharmacological group

Leukotriene receptor antagonist. Drug for the treatment of bronchial asthma and allergic rhinitis

pharmachologic effect

Montelukast is a specific oral leukotriene receptor antagonist. Montelukast has the ability to inhibit inhaled LTD4 bronchospasm at very low doses (5 mg). Bronchodilation is observed within 2 hours after taking the drug inside. The bronchodilation effect caused by beta-agonists is complemented by the action of montelukast. Montelukast inhibits the early and late phases of antigen-induced bronchospasm. Montelukast reduces the number of eosinophils in the peripheral blood, in the respiratory tract (sputum) of adults and children and improves the control of bronchial asthma.

Montelukast significantly improves morning FEV (forced expiratory volume) in 1 s, MOV (maximum expiratory volume flow rate) and significantly reduces the need for beta-agonists.

Montelukast enhances the action of inhaled glucocorticosteroids. Montelukast significantly reduces bronchospasm that occurs during exercise. In patients with bronchial asthma sensitive to acetylsalicylic acid and taking concomitant inhaled and / or oral glucocorticosteroids, treatment with montelukast leads to a significant improvement in the control of asthma symptoms.

Pharmacokinetics

Absorption. Montelukast is rapidly absorbed after oral administration. In adults, when taking 10 mg of montelukast on an empty stomach, Cmax in plasma is reached after 3 hours. On average, bioavailability after oral administration is 64%. Food intake does not affect the bioavailability and C max of montelukast.

Distribution. Montelukast is more than 99% bound to plasma proteins. Vd of montelukast in the equilibrium state averages 8-11 liters. The drug does not penetrate well through the blood-brain barrier. Montelukast concentrations 24 hours after drug administration were minimal in all body tissues.

Biotransformation. Montelukast is extensively metabolized. When using therapeutic doses, the concentration of montelukast metabolites in plasma in an equilibrium state in adults and children is not determined. It is assumed that cytochrome P450 isoenzymes 3A4, 2A6 and 2C9 are involved in the metabolism of montelukast, while at therapeutic concentrations montelukast does not inhibit cytochrome P450 isoenzymes 3A4, 2C9, 1A2, 2A6, 2C19 and 2D6. The contribution of metabolites to the therapeutic effect of montelukast is minimal.

Withdrawal. Plasma clearance of montelukast in healthy adults averages 45 ml/min. After taking montelukast orally, 86% of the drug is excreted through the intestines and less than 0.2% - by the kidneys. The drug and its metabolites are excreted mainly in the bile.

Pharmacokinetics in different groups of patients

For the elderly, patients with mild or moderate hepatic insufficiency, dose adjustment is not required. Studies in patients with renal insufficiency have not been conducted. Since montelukast and its metabolites are excreted in the bile, no dose adjustment is required for patients with renal insufficiency. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic impairment (Child-Pugh score >9 points).

Long-term treatment and prevention of bronchial asthma (including prevention of day and night symptoms of the disease);

Treatment of "aspirin" asthma and prevention of physical effort bronchospasm.

Hypersensitivity to the active substance or to any of the excipients;

Children's age up to 15 years;

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully: pregnancy and lactation.

Blood and lymphatic system disorders: increased tendency to bleed.

Immune system disorders: hypersensitivity reactions, including anaphylaxis; eosinophilic infiltrates of the liver.

Mental disorders: sleep disturbances, including nightmares, hallucinations, insomnia; irritability, anxiety, agitation, including aggressive behavior, tremors, depression, suicidal thoughts and suicidal behavior (suicidality).

Nervous system disorders: headache, dizziness, drowsiness, paresthesia / hypoesthesia, convulsive seizures.

Heart disorders: cardiopalmus.

Gastrointestinal disorders: abdominal pain, diarrhea, dry mouth, dyspepsia, nausea, vomiting.

Hepatobiliary system disorders: increased activity of transaminases in the blood serum (alanine aminotransferase, aspartate aminotransferase), cholestatic hepatitis.

Skin and subcutaneous tissue disorders: angioedema, ecchymosis, urticaria, itching, rash, erythema nodosum.

Musculoskeletal and connective tissue disorders: arthralgia, myalgia, including muscle spasms.

General disorders and disorders at the injection site: thirst, asthenia/increased fatigue, discomfort, swelling.

Churg-Strauss syndrome (systemic eosinophilic vasculitis) has been reported in patients with bronchial asthma while taking montelukast.

Overdose

There is no specific information on the treatment of overdose with Singlon. Data on overdose symptoms when taking the drug by adult patients with bronchial asthma at a dose exceeding 200 mg / day for 22 weeks and at a dose of 900 mg / day for 1 week have not been identified.

There have been cases of acute overdose of montelukast in adults and children at doses above 1000 mg (approximately 61 mg/kg for a child aged 42 months). The obtained clinical and laboratory results were consistent with the safety profile for adults and pediatric patients. The most commonly reported adverse events were consistent with the safety profile of montelukast and included abdominal pain, drowsiness, mydriasis, thirst, headache, vomiting, and psychomotor hyperactivity.

There are no data on the possibility of excretion of montelukast during peritoneal dialysis or hemodialysis.

special instructions

Singlon should not replace inhaled or oral glucocorticosteroids.

There are no data indicating the possibility of reducing the dose of oral glucocorticosteroids with the concomitant use of the drug Singlon.

In rare cases, patients taking drugs for the treatment of bronchial asthma, including the drug Singlon, may experience systemic eosinophilia, sometimes accompanied by clinical manifestations of vasculitis and Churg-Strauss syndrome; this condition is usually treated with systemic glucocorticosteroids. Such cases are usually, but not always, associated with dose reduction or withdrawal of oral glucocorticosteroids. It is impossible to neither exclude nor confirm the possibility that the use of leukotriene receptor antagonists may be associated with the occurrence of Churg-Strauss syndrome. Physicians should be aware of the possibility of patients developing eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy. Patients who develop the above symptoms should be re-evaluated and their treatment regimen should be re-evaluated.

Taking the drug Singlon does not affect the intake of acetylsalicylic acid and other non-steroidal anti-inflammatory drugs in patients with bronchial asthma with hypersensitivity to acetylsalicylic acid.

The drug contains lactose, so it should not be taken by patients with rare hereditary diseases such as lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

The effect of the drug on the ability to drive vehicles and mechanisms

It is assumed that the drug Singlon does not affect the ability to drive a car or other mechanisms. However, in very rare cases, patients have experienced drowsiness.

Elderly

In elderly patients with mild or moderate renal insufficiency, dose adjustment is not required.

Use during pregnancy and lactation

Singlon can be used during pregnancy and lactation if the expected benefit to the mother outweighs the potential risk to the fetus and child.

drug interaction

The drug Singlon can be administered in conjunction with other drugs traditionally prescribed for the prevention and long-term treatment of bronchial asthma. The drug at recommended doses did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol / norethisterone 35/1), terfenadine, digoxin and warfarin.

Plasma AUC of montelukast decreased by approximately 40% in patients treated with montelukast and phenobarbital. Since CYP3A4 is involved in the metabolism of montelukast, caution should be exercised, especially in children, when using montelukast with CYP3A4 inducers such as phenytoin, phenobarbital and rifampicin.

In vitro studies have shown that montelukast is a potent inhibitor of CYP2C8. However, the results of a study of the clinical interaction of montelukast and rosiglitazone (an example of marker substrates for drugs whose main metabolism is carried out by the CYP2C8 enzyme) did not reveal an inhibitory effect of montelukast on CYP2C8 in vivo. Therefore, montelukast is not expected to significantly alter the conversion of drugs that are metabolized by this enzyme (eg, paclitaxel, rosiglitazone, and repaglinide). When taking high doses of montelukast (at 20- and 60-fold excess of the recommended dose for adults), a decrease in the concentration of theophylline in plasma is observed. This effect is not observed when taking the drug in recommended doses - 10 mg / day.

Adults and adolescents aged 15 years and older for the treatment of bronchial asthma, take one tablet of Singlon 10 mg by mouth daily in the evening, with or without food.

The therapeutic effect of the drug Singlon on the symptoms associated with bronchial asthma, manifests itself within one day. The patient is advised to continue taking Singlon both during periods of controlled asthma and during periods of worsening disease.

The drug Singlon should not be taken together with other drugs containing the same active ingredient - montelukast.

In elderly patients with mild or moderate renal insufficiency, hepatic insufficiency dose adjustment is not required. There are no data for patients with severe hepatic impairment.

The dose of the drug is the same for female and male patients.

Singlon can be included in existing asthma treatment regimens.

Inhaled glucocorticosteroids: Singlon is indicated for the treatment of bronchial asthma as adjunctive therapy in patients in whom inhaled glucocorticosteroids and short-acting beta-agonists used as needed do not provide the necessary clinical control of the disease. Montelukast should not replace inhaled glucocorticosteroids.

For children aged 6 to 14 years, 5 mg chewable tablets are used.

Storage conditions and shelf life

Store the drug out of the reach of children, dry and protected from light at a temperature not exceeding 25 ° C. Shelf life - 2 years. Do not use after the expiry date stated on the package.

Active substance

Montelukast (montelukast)

Release form, composition and packaging

Chewable tablets pale yellow, oval, biconvex, with a pronounced cherry smell, blotches of a darker color are allowed; engraved "R13" on one side.

Clinical studies of montelukast in pregnant women have not been conducted. Singlon should be used during pregnancy and lactation only if the expected benefit to the mother outweighs the potential risk to the fetus or child. During the post-registration use of montelukast, the development of congenital limb defects in newborns whose mothers took montelukast during pregnancy has been reported. Most of these women were also taking other asthma medications during pregnancy. A causal relationship between montelukast and the development of congenital limb defects has not been established.

Use in the elderly

In elderly patients, special dose selection is not required.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

The drug should be stored out of the reach of children, in the original packaging, at a temperature not exceeding 25°C. Shelf life - 2 years. Do not use after the expiry date stated on the packaging.

In this article, you can read the instructions for using the drug Singlon. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Singlon in their practice are presented. A big request to actively add your reviews about the drug: did the medicine help or not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Analogues of Singlon in the presence of existing structural analogues. Use for the treatment and prevention of bronchial asthma, including aspirin and bronchospasm in adults, children, as well as during pregnancy and lactation. The composition of the drug.

Singlon- a specific leukotriene receptor antagonist for oral administration. Montelukast (the active ingredient in Singlon) has the ability to inhibit inhaled LTD4 bronchospasm at very low doses (5 mg). Bronchodilation is observed within 2 hours after taking the drug inside. The bronchodilation effect caused by beta-agonists is complemented by the action of montelukast. Singlon inhibits the early and late phases of antigen-induced bronchospasm. Montelukast reduces the number of eosinophils in the peripheral blood, in the respiratory tract (sputum) of adults and children and improves the control of bronchial asthma.

Montelukast significantly improves morning FEV (forced expiratory volume) in 1 second, MOEF (maximum expiratory volume flow rate) and significantly reduces the need for beta-agonists.

Singlon enhances the action of inhaled glucocorticosteroids. Montelukast significantly reduces bronchospasm that occurs during exercise. In patients with bronchial asthma sensitive to acetylsalicylic acid and taking concomitant inhaled and / or oral glucocorticosteroids, treatment with montelukast leads to a significant improvement in the control of asthma symptoms.

Compound

Montelukast sodium + excipients.

Pharmacokinetics

Singlon is rapidly absorbed after oral administration. On average, bioavailability after oral administration is 64%. Eating does not affect bioavailability. Montelukast is more than 99% bound to plasma proteins. The drug does not penetrate well through the blood-brain barrier. Montelukast concentrations 24 hours after drug administration were minimal in all body tissues. Extensively metabolized. When using therapeutic doses, the concentration of montelukast metabolites in plasma in an equilibrium state in adults and children is not determined. The contribution of metabolites to the therapeutic effect of montelukast is minimal. After taking montelukast orally, 86% of the drug is excreted through the intestines and less than 0.2% - by the kidneys. The drug and its metabolites are excreted mainly in the bile.

For the elderly, patients with mild or moderate hepatic insufficiency, dose adjustment is not required.

Indications

long-term treatment and prevention of bronchial asthma (including prevention of day and night symptoms of the disease);
treatment of "aspirin" asthma and prevention of physical effort bronchospasm.

Release form

Film-coated tablets 10 mg.

Chewable tablets 4 mg and 5 mg (children 2-5 years old (4 mg chewable tablets) and children 6-14 years old (5 mg chewable tablets)).

Instructions for use and dosing regimen

Tablets 10 mg

Adults and adolescents aged 15 years and older for the treatment of bronchial asthma, take 1 tablet of Singlon 10 mg orally daily in the evening, with or without food.

The drug Singlon should not be taken together with other drugs containing the same active ingredient - montelukast.

In elderly patients with mild or moderate renal insufficiency, hepatic insufficiency dose adjustment is not required. There are no data for patients with severe hepatic impairment.

The dose of the drug is the same for female and male patients.

Singlon can be included in existing asthma treatment regimens.

Chewable tablets for children

For children aged 2-5 years, Singlon is prescribed 1 chewable tablet 4 mg daily in the evening.

For children aged 6-14 years, Singlon is prescribed 1 chewable tablet 5 mg daily in the evening.

Singlon should be taken 1 hour before or 2 hours after a meal. Dose adjustment within these age groups is not required.

The safety and efficacy of 4 mg chewable tablets in children under 2 years of age has not been established.

The therapeutic effect of the drug Singlon develops within one day after administration. The patient should continue taking Singlon both during periods of controlled asthma and during periods of worsening asthma.

In patients with renal insufficiency, mild or moderate hepatic insufficiency, dose adjustment is not required. There are no data for patients with severe hepatic impairment.

The dose of the drug does not depend on the gender of the patient.

Therapy with Singlon in combination with other drugs for the treatment of bronchial asthma

If Singlon is prescribed while taking inhaled glucocorticosteroids (GCS), then inhaled GCS should not be abruptly replaced with Singlon.

Side effect

increased tendency to bleed;
hypersensitivity reactions, including anaphylaxis;
eosinophilic infiltrates of the liver;
sleep disturbances, including nightmares, hallucinations, insomnia;
irritability;
anxiety;
arousal, including aggressive behavior;
tremor;
depression;
suicidal thoughts and suicidal behavior (suicidality);
headache;
dizziness;
drowsiness;
paresthesia/hypesthesia;
convulsive seizures;
cardiopalmus;
stomach ache;
diarrhea;
dry mouth;
dyspepsia;
nausea, vomiting;
increased activity of transaminases in the blood serum (alanine aminotransferase, aspartate aminotransferase);
cholestatic hepatitis;
angioedema;
the appearance of ecchymosis;
hives;
rash;
nodular erythema;
arthralgia;
myalgia, including muscle spasms;
thirst;
asthenia/increased fatigue;
discomfort;
swelling.

Contraindications

hypersensitivity to the active substance or to any of the excipients;
children's age up to 15 years (for tablets 10 mg);
children's age up to 2 years (for chewable tablets 4 mg);
children's age up to 6 years (for chewable tablets 5 mg);
lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

With caution: pregnancy and lactation.

Use during pregnancy and lactation

Singlon can be used during pregnancy and lactation if the expected benefit to the mother outweighs the potential risk to the fetus and child.

Use in children

Contraindicated in children and adolescents under the age of 15 years.

For children aged 6 to 14 years, 5 mg chewable tablets are used.

For children aged 2 to 5 years, 4 mg chewable tablets are used.

Use in elderly patients

In elderly patients with mild or moderate renal insufficiency, dose adjustment is not required.

special instructions

Singlon should not replace inhaled or oral glucocorticosteroids.

There are no data indicating the possibility of reducing the dose of oral glucocorticosteroids with the concomitant use of the drug Singlon.

The drug contains lactose, so it should not be taken by patients with rare hereditary diseases such as lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

The effect of the drug on the ability to drive vehicles and mechanisms

It is assumed that the drug Singlon does not affect the ability to drive a car or other mechanisms. However, in very rare cases, patients have experienced drowsiness.

drug interaction

Studies have shown that montelukast is a potent inhibitor of CYP2C8. However, the results of a clinical interaction study of montelukast and rosiglitazone (an example of marker substrates for drugs whose main metabolism is carried out by the CYP2C8 enzyme) did not reveal an inhibitory effect of montelukast on CYP2C8. Therefore, montelukast is not expected to significantly alter the conversion of drugs that are metabolized by this enzyme (eg, paclitaxel, rosiglitazone, and repaglinide). When taking high doses of montelukast (at 20- and 60-fold excess of the recommended dose for adults), a decrease in the concentration of theophylline in plasma is observed. This effect is not observed when taking the drug in recommended doses - 10 mg per day.

Analogues of the drug Singlon

Structural analogues for the active substance:

Monax;
Moncasta;
Montelar;
Montelast;
Montelukast;
Simpler;
Syngulex;
Singular;
Ectalust.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.

Compound

Each film-coated tablet contains:

Active substance: montelukast 10 mg (as montelukast sodium 10.4 mg) Excipients:

Nucleus: lactose monohydrate, microcrystalline cellulose 101, hydroxypropylcellulose, croscarmellose sodium, magnesium stearate;

Film sheath: Opadry yellow 20B32427 (hypromellose 3cP, hydroxypropyl cellulose, titanium dioxide (E171), macrogol 400, hypromellose 50cP, iron oxide yellow (E172))

Description

Tablets, film-coated, round biconvex, yellow, with an embossed inscription R 15 on one side, with a diameter of about 8 mm.

Pharmacotherapeutic group

Agents for the treatment of obstructive airway diseases, leukotriene receptor antagonists The codeATX: R03DC03.

Pharmacological properties

Pharmacodynamics

Mechanism of action

Cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids that are released from various cells, including mast cells and eosinophils. These important pro-asthmatic mediators bind to cysteinyl leukotriene (CysLT) receptors. Cysteinyl leukotriene type 1 (CysLT1) receptors are found in the human airways (including smooth muscle cells and lung macrophages) and on the surface of other pro-inflammatory cells (including eosinophils and some myeloid stem cells). CysLT receptors are associated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects develop, including bronchospasm, mucus secretion, vascular permeability, and eosinophil mobilization. In allergic rhinitis, CysLT receptors are released from the nasal mucosa following allergen exposure in both early and late phase reactions; these receptors are associated with symptoms of allergic rhinitis. Intranasal challenge with CysLT receptors increased upper airway resistance and aggravated symptoms of nasal congestion.

Montelukast is an orally active substance that binds with high affinity and selectivity to the CysLT1 receptor.

Clinical efficacy and safety

In clinical studies, montelukast inhibited bronchospasm caused by inhaled LTD4, even at doses as low as 5 mg. Bronchodilation was observed within two hours after ingestion. The bronchodilation effect induced by beta-agonists complemented the bronchodilation effect induced by montelukast. Treatment with montelukast suppressed both early and late antigen-induced bronchospasm. Montelukast reduced the number of eosinophils in the peripheral blood of adults and children compared with placebo. In a separate study, treatment with montelukast resulted in a significant decrease in the number of eosinophils in the respiratory tract (as determined in sputum) and in peripheral blood in both adults and children aged 2 to 14 years, leading to improved clinical control of bronchial asthma.

In studies in adults, montelukast at a dose of 10 mg one laz per day compared with placebo showed a significant improvement in morning forced expiratory volume (FEV1) (change of 10.4% vs. 2.7% compared with baseline), morning peak velocity expiratory flow rate (PSV) (change of 24.5 l/min vs. 3.3 l/min compared to baseline), and a significant decrease in the total use of beta-adrenergic agonists (change of -26.1% vs. -4.6% in compared to the original value). Patient self-reported improvement in daytime and nighttime asthma symptoms was significantly better than placebo.

Studies in adults have shown the ability of montelukast to complement the clinical effect of inhaled glucocorticosteroids (% change from baseline for inhaled beclomethasone in combination with montelukast compared with beclomethasone, respectively, for FEV1: 5.43% vs. 1.04%; use of beta-agonists: - 8.70% versus 2.64%). Compared to inhaled beclomethasone (200 mcg twice daily using a spacer), montelukast showed a faster initial response, although in a 12-week study, beclomethasone provided an average greater treatment effect (% change from baseline for montelukast compared with beclomethasone, respectively, for FEV1: 7.49% vs. 13.3%; use of beta-agonists: - 28.28% vs. -43.89%). However, compared with beclomethasone, a significant percentage of patients treated with montelukast achieved similar clinical efficacy (eg, 50% of patients treated with beclomethasone experienced an improvement in FEV1 of approximately 11% or more from baseline, while about 42% of patients treated with montelukast achieved similar results).

A clinical study was conducted to evaluate the efficacy of montelukast in the symptomatic treatment of concomitant seasonal allergic rhinitis in adult patients and in adolescent patients 15 years of age and older with bronchial asthma. In this study, montelukast tablets 10 mg once daily showed a statistically significant improvement in the Daily Rhinitis Symptoms Rating Scale compared with placebo. Scores on the Diurnal Rhinitis Symptom Rating Scale are the mean of Daily Rhinitis Symptoms (mean of nasal congestion, rhinorrhea, sneezing, and itchy nose) and Nocturnal Rhinitis Symptoms (mean of nasal congestion on waking, difficulty falling asleep, and number of awakenings per day). night time). The overall assessment of symptoms of allergic rhinitis by physicians and patients revealed a significant improvement compared with placebo. Evaluation of efficacy in relation to the treatment of bronchial asthma was not a priority in this study.

In a study in children aged 6 to 14 years lasting 8 weeks, montelukast at a dose of 5 mg once a day compared with placebo significantly improved respiratory function (change in FEV1 by 8.71% vs. 4.16% compared with baseline; change in morning PSV by 27.9 l/min vs. 17.8 l/min compared with baseline) and reduced the need for short-acting beta-adrenergic agonists (change -11.7%: vs. -8.2% compared to e initial value)

In a study in adult patients lasting 12 weeks, a significant reduction in exercise-induced bronchoconstriction was demonstrated (maximum reduction in FEV1 was 22.33% for montelukast vs. 60.64 minutes for placebo). This effect remained unchanged for all 12 weeks. A reduction in exercise-induced bronchoconstriction was also shown in a short-term study in children aged 6 to 14 years (maximum reduction in FEV1 was 18.27% for montelukast versus 26.11% for placebo; the time to recovery from baseline FEV1 ±5% was 17 .76 minutes for montelukast versus 27.98 minutes for placebo). The effect in both studies was achieved at the end of the once-daily dosing interval.

In patients with bronchial asthma sensitive to aspirin and simultaneously receiving therapy with inhaled and / or oral glucocorticosteroids, therapy with montelukast, compared with placebo, led to a significant improvement in the control of symptoms of bronchial asthma (change in FEV1 compared to baseline was 8.55% versus -1 .74%; the decrease in the total need for beta-adrenergic agonists was -27.78% versus 2.09% compared with the initial value).

Pharmacokinetics

Suction

Montelukast is rapidly absorbed after oral administration. For 10 mg film-coated tablets, the average peak plasma concentration (C max) is reached within 3 hours (Tmax) after taking the drug on an empty stomach in adult patients. The average bioavailability after oral administration is 64%. Regular food does not affect oral bioavailability and Cmax. Safety and efficacy have been shown in clinical studies in which 10 mg film-coated tablets were administered without regard to meal times.

For a 5 mg chewable tablet, Cmax is reached two hours after ingestion on an empty stomach by adult patients. The average bioavailability after oral administration is 73% and decreases to 63% after a normal meal.

Distribution and binding to plasma proteins

Montelukast is more than 99% bound to plasma proteins. The volume of distribution of montelukast at steady state averages 8-11 liters. Studies in rats with radiolabeled montelukast show that the penetration of the drug through the blood-brain barrier is minimal. In addition, the concentration of the radioactive label within 24 hours after dosing in all other tissues was minimal.

Metabolism

Montelukast is actively metabolized. In studies with therapeutic doses, the concentration of montelukast metabolites in blood plasma at steady state is below the detection threshold in adults and children.

Cytochrome P4502C8 is the main enzyme involved in the metabolism of montelukast. In addition, CYP3A4 and 2C9 may make a minor contribution, although itraconazole, an inhibitor of CYP3A4, has not been shown to cause changes in the pharmacokinetic parameters of montelukast in healthy subjects who received montelukast at a dose of 10 mg per day. Based on the results of in vitro studies in human liver microsomes, it can be concluded that the therapeutic concentration of montelukast in plasma does not inhibit cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19, or 2D6. The contribution of montelukast metabolites to its therapeutic effect is minimal.

breeding

The mean plasma clearance of montelukast in healthy adults is 45 ml/min. After ingestion of radiolabeled montelukast, 86% of the radioactivity was found in the feces for 5 days and

Pharmacokinetics in selected groups of patients

Dose adjustment in the elderly or in patients with mild to moderate hepatic impairment is not required. No studies have been conducted in patients with renal insufficiency. Due to the fact that montelukast and its metabolites are excreted in the bile, no dose adjustment is expected in patients with renal insufficiency. Data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (Child-Pugh score > 9) have not been received.

When prescribing high doses of montelukast (20 and 60 times the recommended dose for adults), a decrease in theophylline concentration in blood plasma was observed. This effect was not observed when prescribing the recommended dose of 10 mg once a day.

Indications for use

Singlon is indicated for the treatment of bronchial asthma as adjunctive therapy in patients with mild to moderate persistent asthma who are not adequately controlled with inhaled glucocorticosteroids and in whom short-acting beta-adrenomimetics used on demand are unable to provide sufficient clinical control of bronchial asthma.

In those asthmatic patients for whom Singlon is indicated, this medicinal product may also relieve the symptoms of seasonal allergic rhinitis.

Singlon is also indicated for the prevention of asthma attacks when exercise-induced bronchospasm is the predominant component.

Contraindications

Hypersensitivity to the active substance or any of the excipients listed in the Composition section.

Use during pregnancy and during breastfeeding

Pregnancy

No adverse effects on pregnancy or embryonic/fetal development have been found in animal studies.

The limited information from the available pregnancy databases does not suggest a causal relationship between montelukast sodium and malformations (i.e., limb anomalies), which have been reported in rare cases in various countries of the world as part of post-marketing use.

Singlon should only be taken during pregnancy if clearly needed.

Breast-feeding

Studies in rats have shown that montelukast passes into milk. It is not known whether montelukast passes into human breast milk.

The drug Singlon can be administered during feeding only if clearly necessary.

Dosage and administration

The dose for adults and adolescents over 15 years of age with bronchial asthma, or with bronchial asthma and concomitant seasonal allergic rhinitis, is 1 tablet 10 mg once a day in the evening.

If the next dose of the drug is missed, the patient should take the next dose of the drug at the usual time. The patient should not take two consecutive doses.

The therapeutic effect of montelukast on asthma control parameters develops within one day. Montelukast can be taken with or without food. Patients should be advised to continue taking montelukast even during the period of control of bronchial asthma, as well as during periods of exacerbation of bronchial asthma. Singlon should not be taken at the same time as other products containing the same active ingredient, montelukast.

Dose adjustment in the elderly, patients with renal insufficiency, or mild to moderate hepatic insufficiency is not required. There are no reliable data on patients with severe liver failure. The dose for male and female patients is the same.

Treatment with montelukast and other drugs for the treatment of bronchial asthma

Montelukast can be taken in addition to the patient's usual treatment regimen.

Inhaled glucocorticosteroids

Montelukast can be used as adjunctive therapy in patients who do not achieve adequate clinical control on inhaled glucocorticosteroids in combination with short-acting beta-adrenergic agonists used on demand. You should not abruptly replace inhaled glucocorticosteroids with montelukast (see section "Precautions").

Children

The drug Singlon, 10 mg film-coated tablets, is intended for adults and adolescents over 15 years of age.

For children aged 6 to 14 years, 5 mg chewable tablets are available.

For children aged 2 to 5 years, 4 mg chewable tablets are available.

Mode of application

The drug is intended for oral administration in the evening. Singlon, 10 mg film-coated tablets can be taken with or without food.

Side effect

Montelukast was evaluated in clinical studies as follows:

Film-coated tablets, 10 mg - in approximately 4000 adults and adolescents aged 15 years and older with bronchial asthma. film-coated tablets, 10 mg - in approximately 400 adults and adolescents aged 15 years and older with seasonal allergic rhinitis associated with asthma. chewable tablets 5 mg - in approximately 1750 children with bronchial asthma aged 6 to 14 years.

The following drug-related adverse reactions in clinical studies were reported as common (≥ 1/100 to

With long-term treatment in clinical studies with a limited number of patients lasting up to 2 years for adults and up to 12 months for children aged 6 to 14 years, the safety profile did not change.

Post-marketing application

Adverse reactions reported during post-marketing use are listed below by body system classes and terms characterizing adverse events recorded over a long period. Frequency categories were evaluated based on relevant clinical studies.

The following definitions were used to classify the frequency of adverse effects: Very common (≥ 1/10), frequent (≥ 1/100 to

Infections and infestations:

Very common: upper respiratory infections*

Blood and lymphatic system disorders:

Rare: bleeding tendency

Immune system disorders:

Uncommon: hypersensitivity reactions, including anaphylactic reactions

Very rare: eosinophilic infiltration of the liver

Mental disorders:

Infrequent: unusual dreams, including nightmares, insomnia, sleepwalking, anxiety, agitation, including aggressive behavior or hostility, depression, psychomotor agitation (including irritability, restlessness, tremors§)

Rare: impaired attention, memory impairment

Very rare: hallucinations, confusion, suicidal thoughts and behavior (suicidality)

Nervous system disorders:

Uncommon: dizziness, drowsiness, paresthesia/hypoesthesia, convulsions

Heart disorders:

Rare: palpitations

Respiratory, thoracic and mediastinal disorders:

Uncommon: epistaxis

Very rare: Churg-Strauss syndrome (CHS) (see Precautions section), pulmonary eosinophilia

Gastrointestinal disorders:

Frequent: diarrhea**, nausea**, vomiting**

Uncommon: dry mouth, dyspepsia

Hepatobiliary system disorders:

Very rare: Hepatitis (including cholestatic, hepatocellular and mixed liver pattern)

Frequent: increased activity of transaminases (ALT, ACT) in the blood serum

Skin and subcutaneous tissue disorders:

Frequent: rash**

Uncommon: bruising, urticaria, pruritus

Rare: angioedema

Very rare: erythema nodosum, erythema multiforme

Musculoskeletal and connective tissue disorders:

Uncommon: arthralgia, myalgia, including muscle spasms

Systemic disorders and complications at the injection site:

Frequent: fever**

Uncommon: weakness/fatigue, malaise, edema

* This adverse event, reported as very common in patients treated with montelukast, was also reported as very common in patients treated with placebo in clinical trials.

** This adverse event, reported as common in patients treated with montelukast, was also reported as common in patients treated with placebo in clinical trials.

If the listed adverse reactions occur, as well as a reaction not indicated in the instructions, you should consult a doctor.

Overdose

There is no separate information on the treatment of overdose of montelukast. In long-term asthma studies, montelukast has been administered to adult patients at doses up to 200 mg/day for 22 weeks, and in short-term studies at doses up to 900 mg/day for approximately one week without clinically significant adverse events.

Symptoms

There have been reports of acute overdose of montelukast in clinical studies and post-marketing applications. These include reports of doses above 1000 mg in adults and children (approximately 61 mg/kg in a 42-month-old child). Clinical and laboratory parameters were consistent with the safety profile in adults and children. Most reports of overdose did not indicate any adverse events. The most commonly reported adverse events were consistent with the safety profile of montelukast and included abdominal pain, drowsiness, thirst, headache, vomiting, and psychomotor agitation.

It is not known whether montelukast is eliminated by peritoneal dialysis or hemodialysis.

Interaction with other drugs

Montelukast can be taken simultaneously with other drugs for the prevention and treatment of bronchial asthma. In drug interaction studies, the recommended clinical dose of montelukast did not have a clinically significant effect on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (ethinylestradiol/norethindrone ratio 35/1), terfenadine, digoxin and warfarin.

With the simultaneous appointment of phenobarbital, the area under the pharmacokinetic curve "concentration-time" (AUC) for the concentration of montelukast in blood plasma decreased by about 40%. Due to the fact that montelukast is metabolized by the isoenzyme CYP3A4, 2C8 and 2C9, caution should be exercised, especially in children, while prescribing montelukast with inducers of CYP3A4, 2C8 and 2C9 isoenzymes, such as phenytoin, phenobarbital and rifampicin.

In vitro studies have shown that montelukast is a strong inhibitor of the CYP2C8 isoenzyme. However, data from a clinical drug interaction study of montelukast and rosiglitazone (a marker substrate for drugs metabolized mainly by the CYP2C8 isoenzyme) showed that in vivo montelukast does not inhibit the CYP2C8 isoenzyme. Thus, montelukast is not expected to significantly alter the metabolism of drugs metabolized by this enzyme (eg, paclitaxel, rosiglizaton, and repaglinide).

In vitro studies have shown that montelukast is a substrate of the CYP2C8 isoenzyme, and to a lesser extent, a substrate of the 2C9 and 3A4 isoenzymes. In a clinical drug interaction study of montelukast and gemfibrozil (an inhibitor of CYP2C8 and 2C9 isoenzymes), gemfibrozil increased the systemic exposure of montelukast by 4.4 times. Planned dose adjustment of montelukast when administered simultaneously with gemfibrozil or other strong inhibitors of the CYP2C8 isoenzyme is not required, but the doctor should be aware of the possibility of increasing the likelihood of adverse reactions.

Based on data from in vitro studies, it can be concluded that clinically significant drug interactions with less potent inhibitors of the CYP2C8 isoenzyme (for example, trimethoprim) are not expected. Simultaneous administration of montelukast with itraconazole, a strong inhibitor of the CYP3A4 isoenzyme, did not lead to a significant increase in the systemic exposure of montelukast.

Precautionary measures

Patients should be advised not to use oral montelukast for acute asthma attacks and should always carry their usual fast-acting drugs with them. With the development of an acute attack of bronchial asthma, short-acting inhaled beta-agonists should be used. If patients require more breaths of short-acting beta-agonists, they should consult their physician as soon as possible.

Do not abruptly replace inhaled or systemic glucocorticosteroids with montelukast.

No data have been obtained indicating the possibility of reducing the dose of systemic glucocorticosteroids while taking montelukast.

In rare cases, patients receiving anti-asthma drugs, including montelukast, may develop systemic eosinophilia, sometimes with clinical signs of vasculitis consistent with Churg-Strauss syndrome, a condition that often requires therapy with systemic glucocorticosteroids. These events have usually, but not always, been associated with dose reduction or withdrawal of systemic glucocorticosteroids. The possibility that leukotriene receptor antagonists may be associated with the development of Churg-Strauss syndrome cannot be excluded or established. Physicians should be aware of the possibility of developing eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiovascular complications, and/or neuropathy in their patients. If these symptoms develop, patients should be re-examined and their treatment regimens re-evaluated.

Treatment with montelukast does not change the need for patients with aspirin-induced asthma to avoid taking aspirin and other non-steroidal anti-inflammatory drugs.

The tablets contain lactose monohydrate, patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or hereditary malabsorption of glucose and galactose should not take this medicine.

Influence on the ability to drive vehicles and work with mechanisms

Montelukast is not expected to affect the ability to drive and use machines in any way.

However, in very rare cases, patients have reported drowsiness and dizziness.

Package

Manufacturer information

LLC "Gedeon Richter Poland", Grodzisk Mazowiecki, Poland for JSC "Gedeon Richter", Budapest, Hungary.

Company representing the interests of the manufacturer and the applicant:

This page contains a list of all Singlon analogues by composition and indications for use. A list of cheap analogues, and you can also compare prices in pharmacies.

The cheapest analogue of Singlon:
The most popular analogue of Singlon:
ATH classification: Montelukast

Cheap analogues Singlon

When calculating the cost cheap analogues Singlon the minimum price was taken into account, which was found in the price lists provided by pharmacies

Popular analogues Singlon

The list of drug analogues based on the statistics of the most requested drugs

All analogues of Singlon

Analogues in composition and indications for use

Name	Price in Russia	Price in Ukraine
montelukast	--	284 UAH
	--	66 UAH
montelukast	488 rub	184 UAH
montelukast	--	152 UAH
montelukast	299 rub	108 UAH
montelukast	--	--
montelukast	--	33 UAH
montelukast	--	--
montelukast	--	76 UAH
	1832 rub	700 UAH
	--	--
montelukast	157 rub	750 UAH
montelukast sodium	239 rub	412 UAH
montelukast sodium	--	103 UAH
montelukast	--	221 UAH
montelukast	500 rub	750 UAH

The above list of analogues of drugs, which indicates Singlon substitutes, is the most suitable, since they have the same composition of active ingredients and match the indications for use

Different composition, may coincide in indication and method of application

Name	Price in Russia	Price in Ukraine
theophylline	9 rub	3 UAH
theophylline	--	13 UAH
theophylline	124 rub	21 UAH
theophylline	114 rub	28 UAH
theophylline	--	22 UAH
theophylline	--	24 UAH
theophylline	--	3 UAH
theophylline	245 rub	39 UAH
	--	117 UAH
theophylline, potassium chloride, magnesium chloride	--	21 UAH
theophylline, guaifenesin	--	--
belladonna, caffeine, paracetamol, theophylline, phenobarbital, cytisine, ephedrine	--	32 UAH
theophylline, phenobarbital, ephedrine	--	--
fenspiride	--	21 UAH
fenspiride	218 rub	65 UAH
fenspiride	--	32 UAH
fenspiride	--	57 UAH
fenspiride	--	15 UAH
fenspiride hydrochloride	147 rub	--
fenspiride hydrochloride	158 rub	--
fenspiride hydrochloride	146 rub	225 UAH
fenspiride hydrochloride	150 rub	--
fenspiride hydrochloride	--	--
fenspiride	--	36 UAH
omalizumab	17800 rub	6500 UAH
roflumilast	1890 rub	480 UAH
	--	55 UAH

To compile a list of cheap analogues of expensive drugs, we use the prices provided by more than 10,000 pharmacies throughout Russia. The database of medicines and their analogues is updated daily, so the information provided on our website is always up-to-date as of the current day. If you have not found the analogue you are interested in, please use the search above and select the medicine you are interested in from the list. On the page of each of them you will find all possible options for analogues of the desired medicine, as well as prices and addresses of pharmacies in which it is available.

How to find a cheap analogue of an expensive medicine?

To find an inexpensive analogue of a drug, a generic or a synonym, we first of all recommend paying attention to the composition, namely to the same active ingredients and indications for use. The same active ingredients of the drug will indicate that the drug is a synonym for the drug, a pharmaceutical equivalent or a pharmaceutical alternative. However, do not forget about the inactive components of similar drugs, which can affect safety and efficacy. Do not forget about the advice of doctors, self-medication can harm your health, so always consult a doctor before using any medication.

Singlon price

On the sites below you can find prices for Singlon and find out about the availability of a pharmacy nearby

Contraindications

Hypersensitivity, pregnancy, breast-feeding, children's age (up to 6 years).

Use during pregnancy and lactation

Side effects

From the nervous system and sensory organs: unusual vivid dreams, hallucinations, drowsiness, irritability, agitation, including aggressive behavior, fatigue, insomnia, paresthesia/hypesthesia, headache; very rarely - convulsive seizures.

From the digestive tract: nausea, vomiting, dyspepsia, diarrhea, abdominal pain.

From the musculoskeletal system: arthralgia, myalgia, including muscle cramps.

Allergic reactions: anaphylaxis, angioedema, rash, itching, urticaria; very rarely - eosinophilic infiltrates of the liver.

Others: a tendency to increased bleeding, the formation of subcutaneous hemorrhages, palpitations, edema, flu-like syndrome, cough, sinusitis, pharyngitis, increased levels of transaminases.

Precautionary measures

It is necessary to strictly observe the treatment regimen. It is recommended to continue taking it even after a significant improvement has been achieved. Should not be used to relieve acute asthma attacks (does not replace inhaled bronchodilators); when a therapeutic effect appears (usually after the first dose), the number of inhalations of bronchodilators during the day can be reduced.

Singlon ® storage conditions

In a dry, dark place, at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf life of the drug Singlon ®

2 years.

Do not use after the expiry date stated on the packaging.

2000-2015. Register of Medicinal Products of Russia
The database is intended for healthcare professionals.
Commercial use of materials is not permitted.

All information is presented for informational purposes and is not a reason for self-prescription or replacement of the drug.